2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-amine | 943610-63-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-amine
• CAS: 943610-63-7
• 化学式: C₆H₈N₄O₃
• 分子量: 184.155
• InChiKey: SIMHJZHCZNNNEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  98.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-amine 、 3-(3-(4-(trifluoromethoxy)phenoxy)azetidin-1-yl)propionyl chloride 生成 3-(3-(4-(trifluoromethoxy)phenoxy)azetidin-1-yl)-N-((S)-6,7-dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl) propanamide
  参考文献：
  名称：

  (6,7-DIHYDRO-2-NITRO-5H-IMIDAZOL[2,1-B][1,3]OXAZIN-6YL) AMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

  摘要：

  本文揭示了化合物(I) [(6,7-二氢-2-硝基-5H-咪唑[2,1-b][1,3]噁唑-6-基)酰胺]及其药学上可接受的盐、制备方法和制备药物组合物，其中m和R的定义如描述中所述。本文还揭示了该化合物在制备用于治疗由结核分枝杆菌引起的传染病，特别是由多重耐药结核分枝杆菌引起的传染病的药物中的用途。

  公开号：

  US20130143864A1
• 作为产物：
  描述：

  6-azido-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine 在 palladium 10% on activated carbon 氢气 作用下， 以 乙酸乙酯 为溶剂， 反应 2.0h， 以50%的产率得到2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-amine
  参考文献：
  名称：

  WO2007/75872

  摘要：

  公开号：

文献信息

• Nitroimidazole Compound, Preparation Method Therefor And Use Thereof In Drug Manufacturing
  申请人：Shanghai Sun-sail Pharmaceutical Science & Technology Co., Ltd.

  公开号：US20170334927A1

  公开（公告）日：2017-11-23

  A nitroimidazole compound represented by general formula (I) or an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a preparation method therefore, and use thereof in manufacturing drugs for the treating infectious diseases caused by mycobacterium tuberculosis . Specific groups in general formula (I) are as defined in the specification.

  一种由一般式（I）表示的硝基咪唑化合物或其光学异构体或其药学上可接受的盐，以及其制备方法，及其在制造用于治疗由结核分枝杆菌引起的传染病的药物中的用途。一般式（I）中的特定基团如规范中所定义。
• Nitroimidazole Compounds
  申请人：Jiricek Jan

  公开号：US20080275035A1

  公开（公告）日：2008-11-06

  The present invention relates to certain nitroimidazole compounds, which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Mycobacterium tuberculosis, Trypanosoma cruzi or Leishmania donovani . The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.

  本发明涉及某些硝基咪唑化合物，具有有趣的药理特性。特别地，这些化合物在治疗和/或预防由结核分枝杆菌、克鲁兹锥虫或唇鞭毛虫等引起的感染方面是有用的。该发明还涉及含有这些化合物的药物组合物，以及它们的制备方法。
• BICYCLIC NITROIMIDAZOLE-SUBSTITUTED PHENYL OXAZOLIDINONES
  申请人：Ding Charles Z.

  公开号：US20090281088A1

  公开（公告）日：2009-11-12

  The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.

  本发明提供了一系列双环硝基咪唑取代的苯基噁唑烷酮，其中双环硝基咪唑药效团与苯基噁唑烷酮共价键合，它们的制药组合物以及用于预防和治疗细菌感染的组合物的使用方法。这些双环硝基咪唑取代的苯基噁唑烷酮对野生型和耐药菌株具有惊人的抗菌活性，因此对于预防、控制和治疗由这些病原体引起的许多人类和兽医细菌感染是有用的，如结核分枝杆菌。
• (6,7-dihydro-2-nitro-5H-imidazol[2,1-b][1,3]oxazin-6-yl) amide compounds, preparation methods and uses thereof
  申请人：Wang Tiancai

  公开号：US08563547B2

  公开（公告）日：2013-10-22

  (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by Mycobacterium tuberculosis, especially infectious diseases caused by multi-drug resistance Mycobacterium tuberculosi are also disclosed.

  本文介绍了式(I)的(6,7-二氢-2-硝基-5H-咪唑并[2,1-b][1,3]噁唑-6-基)酰胺化合物及其药学上可接受的盐、制备方法和药物组合物，其中m和R的定义如描述中所示。本文还介绍了这些化合物在制备用于治疗由结核分枝杆菌引起的传染病，尤其是由多药耐药结核分枝杆菌引起的传染病的药物中的用途。
• BICYCLIC NITROIMIDAZOLES COVALENTLY LINKED TO SUBSTITUTED PHENYL OXAZOLIDINONES
  申请人：Global Alliance For Tb Drug Development

  公开号：EP2254892A1

  公开（公告）日：2010-12-01